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公开(公告)号:US4808724A
公开(公告)日:1989-02-28
申请号:US103240
申请日:1987-09-30
IPC分类号: A61K31/426 , A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D277/40 , C07D499/00 , C07D499/44 , C07D499/50 , C07D499/52 , C07D501/20 , C07D501/22 , C07D501/36 , C07D501/46 , C07D501/59 , C07F7/08
CPC分类号: C07D277/20 , C07D499/00 , C07F7/0812
摘要: Antibiotically active penicillins and cephalosporins of the formula ##STR1## in which Z is hydrogen or lower alkoxy,n is 1 or 2,Y, in the form of the free acid, is ##STR2## X is --S--, --n--, --SO-- or --SO.sub.2 --, T is an organic radical, hydrogen or halogen,A is hydroxyl, optionally substituted alkyl, a substituted or unsubstituted phenyl ring, an optionally substituted polycyclic aromatic ring, an optionally substituted 5-membered or 6-membered heterocyclic ring with nitrogen, oxygen and/or sulphur as hetero atoms in the ring, or an optionally substituted polycyclic heterocyclic ring,or non-toxic pharmaceutically tolerated salts thereof.
摘要翻译: 其中Z为氢或低级烷氧基的式为“IMAGE”的抗生素活性青霉素和头孢菌素,n为1或2,游离酸形式的Y为-S-,-n-, -SO-或-SO 2 - ,T是有机基团,氢或卤素,A是羟基,任选取代的烷基,取代或未取代的苯基环,任选取代的多环芳环,任选取代的5元或6元 具有氮,氧和/或硫作为杂环原子的杂环,或任选取代的多环杂环,或其无毒的药物耐受盐。
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公开(公告)号:US4344939A
公开(公告)日:1982-08-17
申请号:US154541
申请日:1980-05-29
IPC分类号: C07D499/32 , A61K31/43 , A61P31/04 , C07D499/00 , C07D499/04 , C07D499/44 , C07D499/46 , C07D499/60 , C07D499/64 , C07D499/70 , C07D499/74 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/535 , A61K31/655 , C07D499/52 , C07D499/54 , C07D499/76
CPC分类号: C07D499/00
摘要: New penicillin 1,1-dioxides of the formula ##STR1## or a salt thereof, in which R.sub.1 denotes a hydrogen atom or an ester-forming radical,R.sub.2 denotes a hydrogen atom,R.sub.3 denotes a hydrogen atom,R.sub.4 denotes a hydrogen atom, an optionally substituted naphthyl radical or a radical of the general formula ##STR2## and the remaining variables can be various organic radicals.
摘要翻译: 式(1)所示的新型青霉素1,1-二氧化物或其盐,其中R1表示氢原子或成酯基团,R2表示氢原子,R3表示氢原子,R4表示氢原子, 任选取代的萘基或通式为“IMAGE”的基团,其余的变量可以是各种有机基团。
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公开(公告)号:US5124441A
公开(公告)日:1992-06-23
申请号:US728392
申请日:1985-04-29
IPC分类号: C07D213/71 , C07D213/89 , C07D277/78 , C07D499/00 , C07D499/44 , C07D499/52 , C07H15/252
CPC分类号: C07D213/71 , C07D213/89 , C07D277/78 , C07D499/00 , C07H15/252
摘要: Therapeutically active organic compound exhibiting at least one group comprising a structure --S'--S"--R, wherein the group --S"--R is defined by R being an organic group comprised in a physiologically acceptable compound H--S"--R obtainable by the splitting of the disulfide bridge --S'--S"-- in said structure, in which compound H--S"--R the sulfur atom S" is bound to a carbon atom in a heterocyclic aromatic ring in R having a configuration being such that the compound H--S"--R, while maintaining physiological acceptability, is stabilized, by tautomerism or resonance involving the sulfur atom S" bound to R, so as to be mainly excluded from reaction involving thiol disulfide exchange; S' being bound to an aliphatic carbon atom; and said compound, in addition to the group or groups comprising the structure --S'--S"--R, consisting of a residue of a therapeutically active organic base compound of non-polypeptide structure bound to S'.The invention also relates to a method of modifying a therapeutically active organic compound of non-polypeptide structure by introducing a structure --S'--S"--R according to above; a method of treating diseases by administration of a compound according to the invention and also to a pharmaceutical composition containing at least one compound according to the invention.
摘要翻译: 表现出至少一个包含结构-S'-S“-R的基团的治疗活性有机化合物,其中基团-S”-R由R是由生理上可接受的化合物H-S“ -R可以通过在所述结构中分解二硫键-S'-S'而得到,其中化合物H-S“-R是硫原子S”与杂环芳环中的碳原子结合 R具有使得化合物H-S“-R'同时保持生理可接受性的稳定性,通过涉及与R结合的硫原子S”的互变异构体或共振,从而主要排除在涉及硫醇的反应之外 二硫化物交换; S'与脂肪族碳原子结合; 和所述化合物,除了包含结构-S'-S“-R”的基团或基团,由与S'结合的非多肽结构的治疗活性有机碱性化合物的残基组成。 本发明还涉及通过引入上述结构-S'-S“-R修饰非多肽结构的治疗活性有机化合物的方法; 通过施用根据本发明的化合物治疗疾病的方法,还涉及含有至少一种本发明化合物的药物组合物。
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公开(公告)号:US4735938A
公开(公告)日:1988-04-05
申请号:US884328
申请日:1986-07-10
IPC分类号: A61K31/426 , A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D277/40 , C07D499/00 , C07D499/44 , C07D499/50 , C07D499/52 , C07D501/20 , C07D501/22 , C07D501/36 , C07D501/46 , C07D501/59 , C07F7/08
CPC分类号: C07D277/20 , C07D499/00 , C07F7/0812
摘要: Antibiotically active penicillins and cephalosporins of the formula ##STR1## in which Z is hydrogen or lower alkoxy,n is 1 or 2,Y, in the form of the free acid, is ##STR2## X is --S--, --n--, --SO-- or --SO.sub.2 --, T is an organic radical, hydrogen or halogen,A is hydroxyl, optionally substituted alkyl, a substituted or unsubstituted phenyl ring, an optionally substituted polycyclic aromatic ring, an optionally substituted 5-membered or 6-membered heterocyclic ring with nitrogen, oxygen and/or sulphur as hetero atoms in the ring, or an optionally substituted polycyclic heterocyclic ring,or non-toxic pharmaceutically tolerated salts thereof.
摘要翻译: 其中Z为氢或低级烷氧基的式为“IMAGE”的抗生素活性青霉素和头孢菌素,n为1或2,游离酸形式的Y为-S-,-n-, -SO-或-SO 2 - ,T是有机基团,氢或卤素,A是羟基,任选取代的烷基,取代或未取代的苯基环,任选取代的多环芳环,任选取代的5元或6元 具有氮,氧和/或硫作为杂环原子的杂环,或任选取代的多环杂环,或其无毒的药物耐受盐。
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